Preparation and use of bicyclic himbacine derivatives as PAR-1 receptor antagonists

US9340530B2 · kind B2 · utility

Assignee

• Merck Sharp & Dohme LLC · US

Inventors

• Mihir Mandal · Westfield, US
• Timothy A. Blizzard · Middletown, US
• Helen Chen · Livingston, US
• Harry R. Chobanian · Kenilworth, US
• Yan Guo · Westfield, US
• Barbara Pio · West Orange, US
• Zhicai Wu · Montvale, US
• Tesfaye Biftu · Belmont, US
• William J. Greenlee · Teaneck, US
• Johnny Zhaoning Zhu · Slough, GB

Key dates

• Filing date: Feb 27, 2013
• Grant date: May 17, 2016
• Expiry date: Feb 27, 2033

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D417/14
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

The present invention relates to bicyclic himbacine derivatives of the formula or a pharmaceutically acceptable salt thereof, wherein: X is —O—, —N(R), —C(R8)(R9) or —C(O)—; and Y is —O—, —N(R), —C(R8)(R9) or —C(O)— and the remaining variables are described herein. The compounds of the invention are effective inhibitors of the PAR-1 receptor. The inventive compounds may be used for the treatment or prophylaxis of disease states such as ACS, secondary prevention of myocardial infarction or stroke, or PAD.